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Assay Detail

CHEMBL3749133

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Agonist activity at human FXR transfected in HEK293 cells assessed as transcriptional activity by luciferase reporter gene assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Bile acid receptor (CHEMBL2047)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 6-(4-{[5-Cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl]methoxy}piperidin-1-yl)-1-methyl-1H-indole-3-carboxylic Acid: A Novel FXR Agonist for the Treatment of Dyslipidemia.
Genin MJ, Bueno AB, Agejas Francisco J, Manninen PR, Bocchinfuso WP, Montrose-Rafizadeh C, Cannady EA, Jones TM, Stille JR, Raddad E, Reidy C, Cox A, Michael MD, Michael LF.
J Med Chem (2015) 58 : 9768 -9772
PubMed 26568144 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 6.57 6.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3746388 TERN-101 2.0 1 6.71
CHEMBL318457 1 6.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3746388 TERN-101 EC50 = 193.0 nM 6.71
CHEMBL318457 EC50 = 373.0 nM 6.43